1. Epigenetics
  2. Histone Methyltransferase
  3. SGC0946

SGC0946 

Cat. No.: HY-15650 Purity: 99.68%
Handling Instructions

SGC0946 is a highly potent and selective DOT1L methyltransferase inhibitor with IC50 of 0.3 nM; selectively kill mixed lineage leukaemia cells.

For research use only. We do not sell to patients.

SGC0946 Chemical Structure

SGC0946 Chemical Structure

CAS No. : 1561178-17-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 98 In-stock
Estimated Time of Arrival: December 31
5 mg USD 72 In-stock
Estimated Time of Arrival: December 31
10 mg USD 126 In-stock
Estimated Time of Arrival: December 31
50 mg USD 504 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

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Description

SGC0946 is a highly potent and selective DOT1L methyltransferase inhibitor with IC50 of 0.3 nM; selectively kill mixed lineage leukaemia cells. IC50 value: 0.3 nM(DOT1L) [1] Target: selective DOT1L inhibitor SGC 0946 is over 100-fold selective for other histone methyltransferases/HMTs. SGC 0946 potently reduces H3K79 dimethylation with IC50 of 2.6 nM in A431 cells, and 8.8 nM in MCF10A cells, which potently and selectively kills cells containing an MLL translocation. SGC 0946 is much more potent than its close analog EPZ004777, and serves as an excellent chemical probe for investigating DOT1L and further development of DOT1L inhibitors for cancer therapy.

Molecular Weight

618.57

Formula

C₂₈H₄₀BrN₇O₄

CAS No.

1561178-17-3

SMILES

NC1=NC=NC2=C1C(Br)=CN2[[email protected]]3[[email protected]](O)[[email protected]](O)[[email protected]@H](CN(CCCNC(NC4=CC=C(C(C)(C)C)C=C4)=O)C(C)C)O3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 33 mg/mL (53.35 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6166 mL 8.0832 mL 16.1663 mL
5 mM 0.3233 mL 1.6166 mL 3.2333 mL
10 mM 0.1617 mL 0.8083 mL 1.6166 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (4.04 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (4.04 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.04 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.68%

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Keywords:

SGC0946SGC 0946SGC-0946Histone MethyltransferaseInhibitorinhibitorinhibit

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SGC0946
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